摘要
依据药物化学中的拼合原理,本文设计了3个吲哚布芬四氢异喹啉衍生物,通过氯化反应、酰胺化反应、Bischler-Napieralski反应等步骤对设计化合物进行了合成,所合成目标化合物均经~1H-NMR、~(13)C-NMR、MS谱图佐证。采用Born比浊法测试了所合成目标化合物体外抗血小板聚集活性,其中化合物8b对AA和ADP诱导的血小板聚集显示了较好的活性,其IC50为1. 7 mmol·L~(-1)和6. 2 mmol·L~(-1),均优于阳性对照药阿司匹林。
Three indobufen tetrahydroisoquinoline derivatives based on combination principles were designed. They were synthesized by reaction chlorination,acylation reaction and Bischler-Napieralski reaction. The structures of three derivatives were identified by ~1H-NMR,~(13)C-NMR,MS. The targets compounds were tested for antiplatelet aggregation by Born turbidimetry method. The compound 8b showed a better activity against AA and ADP inducing platelet aggregation than aspirin,the IC50 value were 1. 7 mmol·L~(-1)and 6. 2mmol·L~(-1).
引文
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